BRPI0710979A2 - composto, composição farmacêutica, uso de um composto, métodos para a inibição de relaxamentos do esfìncter esofágico inferior transitórios e para o tratamento ou prevenção de doença e de condição, e, combinação - Google Patents

composto, composição farmacêutica, uso de um composto, métodos para a inibição de relaxamentos do esfìncter esofágico inferior transitórios e para o tratamento ou prevenção de doença e de condição, e, combinação Download PDF

Info

Publication number: BRPI0710979A2
Authority: BR; Brazil
Prior art keywords: methyl; phenyl; pyrrolidin; isoxazol; triazol
Prior art date: 2006-05-05

Application number

BRPI0710979-2A

Other languages

English (en)

Portuguese (pt)

Inventor

Andreas Wallberg

Karolina Nilsson

Bjoern Holm

Mats Nagard

Kenneth Granberg

Abdelmalik Slassi

Louise Edwards

Methvin Isaac

Tao Xin

Tomislav Stefanac

Original Assignee

Astrazeneca Ab

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2006-05-05

Filing date

2007-04-25

Publication date

2011-05-31

2007-04-25 Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab

2011-05-31 Publication of BRPI0710979A2 publication Critical patent/BRPI0710979A2/pt

Links

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-1 5- { (R) -2- [2- (3-Chloro-phenyl) -2H-tetrazol-5-yl] -pyrrolidin-1-yl} -4-methyl-4H- [1,2,4] triazol-3-one Chemical compound 0.000 claims description 49
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MNTZZDOKIWMNIM-UHFFFAOYSA-N phenyl cyclopropanecarboxylate Chemical compound C1CC1C(=O)OC1=CC=CC=C1 MNTZZDOKIWMNIM-UHFFFAOYSA-N 0.000 description 1
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150000003077 polyols Chemical class 0.000 description 1
229920001155 polypropylene Polymers 0.000 description 1
CHKVPAROMQMJNQ-UHFFFAOYSA-M potassium bisulfate Chemical compound [K+].OS([O-])(=O)=O CHKVPAROMQMJNQ-UHFFFAOYSA-M 0.000 description 1
229910000343 potassium bisulfate Inorganic materials 0.000 description 1
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230000003389 potentiating effect Effects 0.000 description 1
239000002244 precipitate Substances 0.000 description 1
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NIPZZXUFJPQHNH-UHFFFAOYSA-N pyrazine-2-carboxylic acid Chemical compound OC(=O)C1=CN=CC=N1 NIPZZXUFJPQHNH-UHFFFAOYSA-N 0.000 description 1
JUSIWJONLKBPDU-UHFFFAOYSA-N pyridazine-4-carboxylic acid Chemical compound OC(=O)C1=CC=NN=C1 JUSIWJONLKBPDU-UHFFFAOYSA-N 0.000 description 1
150000003242 quaternary ammonium salts Chemical class 0.000 description 1
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230000027425 release of sequestered calcium ion into cytosol Effects 0.000 description 1
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238000004366 reverse phase liquid chromatography Methods 0.000 description 1
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230000002441 reversible effect Effects 0.000 description 1
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229910052708 sodium Inorganic materials 0.000 description 1
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239000012312 sodium hydride Substances 0.000 description 1
229960001922 sodium perborate Drugs 0.000 description 1
229940056729 sodium sulfate anhydrous Drugs 0.000 description 1
229910001495 sodium tetrafluoroborate Inorganic materials 0.000 description 1
YKLJGMBLPUQQOI-UHFFFAOYSA-M sodium;oxidooxy(oxo)borane Chemical compound [Na+].[O-]OB=O YKLJGMBLPUQQOI-UHFFFAOYSA-M 0.000 description 1
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229910052623 talc Inorganic materials 0.000 description 1
229940095064 tartrate Drugs 0.000 description 1
KEKOWHLHSVLJLH-SSDOTTSWSA-N tert-butyl (2r)-2-(2h-tetrazol-5-yl)pyrrolidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC[C@@H]1C1=NNN=N1 KEKOWHLHSVLJLH-SSDOTTSWSA-N 0.000 description 1
FBKDHUOQMIGIED-SECBINFHSA-N tert-butyl (2r)-2-(hydroxyiminomethyl)piperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCCC[C@@H]1C=NO FBKDHUOQMIGIED-SECBINFHSA-N 0.000 description 1
PITJAAIPVBVRAO-SSDOTTSWSA-N tert-butyl (2r)-2-carbamoylpyrrolidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC[C@@H]1C(N)=O PITJAAIPVBVRAO-SSDOTTSWSA-N 0.000 description 1
KZNDGAGWQPGYTB-SECBINFHSA-N tert-butyl (2r)-2-formylpiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCCC[C@@H]1C=O KZNDGAGWQPGYTB-SECBINFHSA-N 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 1
210000001103 thalamus Anatomy 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
239000002562 thickening agent Substances 0.000 description 1
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210000001519 tissue Anatomy 0.000 description 1
JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
239000000196 tragacanth Substances 0.000 description 1
235000010487 tragacanth Nutrition 0.000 description 1
229940116362 tragacanth Drugs 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
238000010361 transduction Methods 0.000 description 1
230000026683 transduction Effects 0.000 description 1
229910052723 transition metal Inorganic materials 0.000 description 1
150000003624 transition metals Chemical class 0.000 description 1
MPSUGQWRVNRJEE-UHFFFAOYSA-N triazol-1-amine Chemical class NN1C=CN=N1 MPSUGQWRVNRJEE-UHFFFAOYSA-N 0.000 description 1
150000003852 triazoles Chemical class 0.000 description 1
YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
230000001960 triggered effect Effects 0.000 description 1
SEDZOYHHAIAQIW-UHFFFAOYSA-N trimethylsilyl azide Chemical compound C[Si](C)(C)N=[N+]=[N-] SEDZOYHHAIAQIW-UHFFFAOYSA-N 0.000 description 1
239000001226 triphosphate Substances 0.000 description 1
235000011178 triphosphate Nutrition 0.000 description 1
UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 description 1
230000017260 vegetative to reproductive phase transition of meristem Effects 0.000 description 1
239000003981 vehicle Substances 0.000 description 1
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235000019786 weight gain Nutrition 0.000 description 1
229910052725 zinc Inorganic materials 0.000 description 1
239000004246 zinc acetate Substances 0.000 description 1
GTLDTDOJJJZVBW-UHFFFAOYSA-N zinc cyanide Chemical compound [Zn+2].N#[C-].N#[C-] GTLDTDOJJJZVBW-UHFFFAOYSA-N 0.000 description 1

Classifications

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BRPI0710979-2A 2006-05-05 2007-04-25 composto, composição farmacêutica, uso de um composto, métodos para a inibição de relaxamentos do esfìncter esofágico inferior transitórios e para o tratamento ou prevenção de doença e de condição, e, combinação BRPI0710979A2 (pt)

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US79765906P	2006-05-05	2006-05-05
US60/797659		2006-05-05
PCT/US2007/067367 WO2007130820A2 (en)	2006-05-05	2007-04-25	Mglur5 modulators i

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US (1)	US7678796B2 (es)
EP (1)	EP2027120A2 (es)
JP (1)	JP2009536209A (es)
KR (1)	KR20090009952A (es)
CN (1)	CN101506202A (es)
AR (1)	AR060651A1 (es)
AU (1)	AU2007248288A1 (es)
BR (1)	BRPI0710979A2 (es)
CA (1)	CA2650114A1 (es)
CL (1)	CL2007001174A1 (es)
CO (1)	CO6140060A2 (es)
EC (1)	ECSP088864A (es)
IL (1)	IL194814A0 (es)
MX (1)	MX2008013835A (es)
NO (1)	NO20084850L (es)
RU (1)	RU2008141509A (es)
TW (1)	TW200811157A (es)
UY (1)	UY30304A1 (es)
WO (1)	WO2007130820A2 (es)

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SG149900A1 (en) *	2004-02-18	2009-02-27	Astrazeneca Ab	Polyheterocyclic compounds and their use as metabotropic glutamate receptor antagonists
TW200821305A (en) *	2006-10-05	2008-05-16	Astrazeneca Ab	MGluR5 modulators
GEP20125425B (en) *	2006-10-18	2012-03-26	Pfizer Prod Inc	Biaryl ether urea compounds
ES2655466T3 (es)	2007-08-13	2018-02-20	Monsanto Technology Llc	Composiciones y procedimientos de control de nematodos
BRPI0818448A2 (pt)	2007-10-19	2015-05-12	Astrazeneca Ab	Composto, composição farmacêutica, uso de um composto, e, métodos para o tratamento ou prevenção de um distúrbio madiano pelo receptor mglur5.
WO2009054785A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	1,2,4-triazole ether derivatives as modulators of mglur5
WO2009054786A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	1,2,4-triazole aryl n-oxides derivatives as modulators of mglur5
CA2702974A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	Amino 1,2,4-triazole derivatives as modulators of mglur5
WO2009054789A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	1,2,3-triazole pyrrolidine derivatives as modulators of mglur5
WO2009054791A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	Fused pyrrolidine 1,2,4-triazole derivatives as modulators of mglur5
WO2009054790A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	Amide linked heteroaromatic derivatives as modulators of mglur5
WO2009054787A1 (en) *	2007-10-26	2009-04-30	Astrazeneca Ab	1,2,4-triazole carboxylic acid derivatives as modulators of mglur5
TW200922586A (en) *	2007-10-26	2009-06-01	Astrazeneca Ab	Thiophene 1,2,4-triazole derivatives as modulators of mGluR5
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- 2007-04-25 CA CA002650114A patent/CA2650114A1/en not_active Abandoned
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- 2007-04-25 JP JP2009509953A patent/JP2009536209A/ja active Pending
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- 2007-04-25 AU AU2007248288A patent/AU2007248288A1/en not_active Abandoned
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- 2007-04-25 UY UY30304A patent/UY30304A1/es not_active Application Discontinuation
- 2007-04-25 WO PCT/US2007/067367 patent/WO2007130820A2/en not_active Ceased
- 2007-04-25 CL CL2007001174A patent/CL2007001174A1/es unknown
- 2007-04-25 KR KR1020087029720A patent/KR20090009952A/ko not_active Withdrawn
- 2007-04-25 AR ARP070101781A patent/AR060651A1/es unknown
- 2007-04-25 CN CNA2007800252941A patent/CN101506202A/zh active Pending
2008
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CA2650114A1 (en)	2007-11-15
KR20090009952A (ko)	2009-01-23
CN101506202A (zh)	2009-08-12
CL2007001174A1 (es)	2008-01-18
US20070259862A1 (en)	2007-11-08
JP2009536209A (ja)	2009-10-08
NO20084850L (no)	2008-12-02
EP2027120A2 (en)	2009-02-25
IL194814A0 (en)	2009-08-03
CO6140060A2 (es)	2010-03-19
MX2008013835A (es)	2008-11-10
US7678796B2 (en)	2010-03-16
AU2007248288A1 (en)	2007-11-15
TW200811157A (en)	2008-03-01
UY30304A1 (es)	2007-11-30
ECSP088864A (es)	2008-12-30
AR060651A1 (es)	2008-07-02
RU2008141509A (ru)	2010-06-20
WO2007130820A3 (en)	2008-03-13
WO2007130820A2 (en)	2007-11-15

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2012-11-13	B08K	Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]	Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 5A ANUIDADE.

Publication	Publication Date	Title
US7678796B2 (en)	2010-03-16	MGluR5 modulators I
AU2007303889B2 (en)	2011-02-24	mGluR5 modulators
US20070259926A1 (en)	2007-11-08	mGluR5 modulators III
KR20070052693A (ko)	2007-05-22	폴리헤테로시클릭 화합물 및 대사성 글루타메이트 수용체길항제로서 이들의 용도
BRPI0710980A2 (pt)	2011-05-31	composto, composição farmacêutica, uso de um composto, métodos para a inibição de relaxamentos do esfìncter esofágio inferior transitórios, para o tratamento ou prevenção de uma doença ou condição, e, combinação
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US20070259923A1 (en)	2007-11-08	MGluR5 modulators IV
US20070259916A1 (en)	2007-11-08	mGluR5 modulators II
US20090111820A1 (en)	2009-04-30	Fused pyrrolidine 1,2,4-triazole derivatives as modulators of mglur5
US20090111825A1 (en)	2009-04-30	Thiophene 1,2,4-triazole derivatives as modulators of mglur5
US20090111822A1 (en)	2009-04-30	1,2,3-triazole pyrrolidine derivatives as modulators of mglur5
US20090111854A1 (en)	2009-04-30	1,2,4-triazole aryl n-oxides derivatives as modulators of mglur5
US20090111823A1 (en)	2009-04-30	Aminopyridine derivatives as modulators of mglur5